Ono Masahiro
Department of Patho-Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan.
Yakugaku Zasshi. 2009 Mar;129(3):279-87. doi: 10.1248/yakushi.129.279.
Molecular imaging by PET/SPECT with radiopharmaceuticals enables noninvasively quantitative evaluation of physiological function, gene expression, pharmacokinetics of proteins and peptides and distribution of receptors with high sensitivity. Together with recent development of imaging equipments, molecular imaging by PET/SPECT is expected to contribute to elucidation of physiological and pathological functions, medical sciences and clinical diagnoses. Molecular imaging with radiopharmaceuticals started from diagnosis of cancer with (18)F-2-fluoro-2-deoxyglucose ([(18)F]FDG). Currently, [(18)F]FDG is commonly used in the field of clinical diagnosis, because it can provide qualitative information on malignancy and metastasis of tumor. Since its achievement, much effort has been devoted to the development of radiopharmaceuticals that bind or interact with the in vivo biomarkers. For example, a number of radiopharmaceuticals based on proteins and peptides with high binding affinities to various biomarkers have been applied for the diagnosis of tumor, arteriosclerosis, thrombus and so on. Furthermore, Alzheimer's disease is also a major target for diagnosis by PET/SPECT imaging. The development of low-molecular-weight radiolabeled probes for the quantitation of beta-amyloid plaques and neurofibrillary tangles in Alzheimer's brains is a topic of current PET/SPECT imaging studies. Here, some recent progress and development of radiopharmaceuticals for PET/SPECT imaging will be reviewed.
利用放射性药物通过正电子发射断层扫描(PET)/单光子发射计算机断层扫描(SPECT)进行分子成像,能够以高灵敏度对生理功能、基因表达、蛋白质和肽的药代动力学以及受体分布进行无创定量评估。随着成像设备的不断发展,PET/SPECT分子成像有望为阐明生理和病理功能、医学科学以及临床诊断做出贡献。放射性药物分子成像始于用(18)F - 2 - 氟 - 2 - 脱氧葡萄糖([(18)F]FDG)诊断癌症。目前,[(18)F]FDG在临床诊断领域被广泛应用,因为它能提供有关肿瘤恶性程度和转移的定性信息。自其问世以来,人们在开发与体内生物标志物结合或相互作用的放射性药物方面投入了大量精力。例如,许多基于与各种生物标志物具有高结合亲和力的蛋白质和肽的放射性药物已被应用于肿瘤、动脉硬化、血栓等疾病的诊断。此外,阿尔茨海默病也是PET/SPECT成像诊断的主要目标。开发用于定量阿尔茨海默病大脑中β - 淀粉样斑块和神经原纤维缠结的低分子量放射性标记探针是当前PET/SPECT成像研究的一个课题。在此,将对PET/SPECT成像放射性药物的一些最新进展和发展进行综述。